アミノアルコール有機分子触媒不斉Diels‐Alder反応を鍵反応とする新規抗インフルエンザ活性物質の合成研究アミノアルコール有機分子触媒不斉Diels‐Alder反応を鍵反応とする新規抗インフルエンザ活性物質の合成研究AA1208032XDevelopment or new anti-influenza molecules using organocatalyzed Diels-Alder reaction of 1,2-dihydropyridines with dienophiles as a key reaction

Tamiflu is a potent inhibitory neuraminidase that is used worldwide as a drug for influenza. However, most recently, a microbe resistant to Tamiflu was confirmed. Therefore, the development of an effective new anti-influenza molecules is needed as soon as possible. In this study, we tried to prepare a new antiviral candidate molecules having the characteristic of both Tamiflu and Relenza by using amino alcohol organocatalyzed DA reaction of 1,2-dihydropyridines with acrolein as a key reaction. We will describe that the synthesis of both the key intermediates 5 and 6 that were obtained from the chiral isoquinuclidine deriveative 3, and the preparation of new antiviral candidate molecules X, Y derived from 5, 6 and its anti-influenza activety.2P-14